Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB

ACS Chemical Biology

Volumn 6, Issue 2, 2011, Pages 131-134

  Kojetin, Douglas ^a   Wang, Yongjun ^a   Kamenecka, Theodore M ^a   Burris, Thomas P ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GLUCOSE 6 PHOSPHATASE; GSK 4112; HEME; NUCLEAR RECEPTOR NR1D1; PHOSPHOENOLPYRUVATE CARBOXYKINASE (GTP); PROTEIN BMAL1; SR 8278; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CHEMICAL STRUCTURE; CONTROLLED STUDY; DRUG IDENTIFICATION; GENE EXPRESSION; GENE FUNCTION; GENE TARGETING; GLUCONEOGENESIS; IN VITRO STUDY; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CELLS, CULTURED; CO-REPRESSOR PROTEINS; DNA, COMPLEMENTARY; DOSE-RESPONSE RELATIONSHIP, DRUG; GLUCONEOGENESIS; HEK293 CELLS; HEME; HUMANS; ISOQUINOLINES; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP D, MEMBER 1; POLYMERASE CHAIN REACTION; PROTEASE INHIBITORS; THIOPHENES;

EID: 79951908010     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb1002575     Document Type: Article

References (12)

1. Raghuram, S., Stayrook, K. R., Huang, P., Rogers, P. M., Nosie, A. K., McClure, D. B., Burris, L. L., Khorasanizadeh, S., Burris, T. P., and Rastinejad, F. (2007) Identification of heme as the ligand for the orphan nuclear receptors REV-ERB[alpha] and REV-ERB[beta] Nat. Struct. Mol. Biol. 14, 1207-1213
2. Yin, L., Wu, N., Curtin, J. C., Qatanani, M., Szwergold, N. R., Reid, R. A., Waitt, G. M., Parks, D. J., Pearce, K. H., Wisely, G. B., and Lazar, M. A. (2007) Rev-erb{alpha}, a heme sensor that coordinates metabolic and circadian pathways Science 318, 1786-1789
3. Guillaumond, F., Dardente, H., Giguere, V., and Cermakian, N. (2005) Differential control of Bmal1 circadian transcription by REV-ERB and ROR nuclear receptors J. Biol. Rhythms 20, 391-403
4. Preitner, N., Damiola, F., Molina, L. L., Zakany, J., Duboule, D., Albrecht, U., and Schibler, U. (2002) The orphan nuclear receptor REV-ERB alpha controls circadian transcription within the positive limb of the mammalian circadian oscillator Cell 110, 251-260
5. Chawla, A. and Lazar, M. A. (1993) Induction of REV-ERBA-alpha, an orphan receptor encoded on the opposite strand of the alpha-thyroid hormone-receptor gene, during adipocyte differentiation J. Biol. Chem. 268, 16265-16269
6. Raspe, E., Mautino, G., Duez, H., Fruchart, J. C., and Staels, B. (2001) Transcriptional regulation of apolipoprotein C-III gene expression by the orphan nuclear receptor Rev-erb alpha Circulation 104, 15-15
7. Duez, H., Van Der Veen, J. N., Duhem, C., Pourcet, B., Touvier, T., Fontaine, C., Derudas, B., Bauge, E., Havinga, R., Bloks, V. W., Wolters, H., Van Der Sluijs, F. H., Vennstrom, B., Kuipers, F., and Staels, B. (2008) Regulation of bile acid synthesis by the nuclear receptor Rev-erb alpha Gastroenterology 135, 689-698
8. Meng, Q. J., McMaster, A., Beesley, S., Lu, W. Q., Gibbs, J., Parks, D., Collins, J., Farrow, S., Donn, R., Ray, D., and Loudon, A. (2008) Ligand modulation of REV-ERB{alpha} function resets the peripheral circadian clock in a phasic manner J. Cell Sci. 121, 3629-3635
9. Kumar, N., Solt, L. A., Wang, Y., Rogers, P. M., Bhattacharyya, G., Kamenecka, T. M., Stayrook, K. R., Crumbley, C., Floyd, Z. E., Gimble, J. M., Griffin, P. R., and Burris, T. P. (2010) Regulation of adipogenesis by natural and synthetic REV-ERB ligands, Endocrinology Published online April 28, 2010; DOI: 10.1210/en.2009-0800.
10. Raghuram, S., Stayrook, K. R., Huang, P., Rogers, P. M., Nosie, A. K., McClure, D. B., Burris, L. L., Khorasanizadeh, S., Burris, T. P., and Rastinejad, F. (2007) Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta Nat. Struct. Mol. Biol. 14, 1207-1213
11. Grant, D., Yin, L., Collins, J. L., Parks, D. J., Orband-Miller, L. A., Wisely, G. B., Joshi, S., Lazar, M. A., Willson, T. M., and Zuercher, W. J. (2010) GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erb alpha ACS Chem. Biol. 5, 925-932
12. Kumar, N., Solt, L. A., Conkright, J. J., Wang, Y., Istrate, M. A., Busby, S. A., Garcia-Ordonez, R., Burris, T. P., and Griffin, P. R. (2010) The benzenesulfonamide T0901317 is a novel ROR{alpha}/{gamma} inverse agonist Mol. Pharmacol. 77, 228-236